sphingosine-1-phosphate receptor subtype 1 (S1PR1 or S1P1), also called endothelial differentiation gene 1 (Edg1), member of the class A family of seven-transmembrane G protein-coupled receptors
The endothelial differentiation gene (Edg) family of G-protein coupled receptors binds blood borne lysophospholipids including sphingosine-1-phosphate (S1P) and lysophosphatidic acid (LPA), which are involved in the regulation of cell proliferation, survival, migration, invasion, endothelial cell shape change and cytoskeletal remodeling. The Edg receptors are classified into two subfamilies: the lysophosphatidic acid subfamily that includes LPA1 (Edg2), LPA2 (Edg4), and LPA3 (Edg7); and the S1P subfamily that includes S1P1 (Edg1), S1P2 (Edg5), S1P3 (Edg3), S1P4 (Edg6), and S1P5 (Edg8). The Edg receptors couple and activate at least three different G protein subtypes including G(i/o), G(q/11), and G(12/13).
Feature 1:ligand binding site [chemical binding site]
Evidence:
Structure:3V2Y: Human lipid-sensing GPCR, the S1P1 receptor fused to T4-lysozyme, in complex with the selective antagonist sphingolipid mimic (R)-3-amino-(3-hexylphenylamino)-4-oxobutylphosphonic acid (ML056), contacts at 4A.
Jiyao W et al.(2023). "The conserved domain database in 2023.",